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Assay Detail

CHEMBL4351081

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells after 80 mins by fluorescence polarization assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

PI3-kinase p110-delta/p85-alpha (CHEMBL2111432)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Evolution of PI3Kγ and δ Inhibitors for Inflammatory and Autoimmune Diseases.
Perry MWD, Abdulai R, Mogemark M, Petersen J, Thomas MJ, Valastro B, Westin Eriksson A.
J Med Chem (2019) 62 : 4783 -4814
PubMed 30582813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.96 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4438249 AMDIZALISIB 2.0 1 9.52
CHEMBL4441870 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4438249 AMDIZALISIB IC50 = 0.3 nM 9.52
CHEMBL4441870 IC50 = 4.0 nM 8.40